CA3112808A1 - Systeme d'administration transdermique de medicament - Google Patents
Systeme d'administration transdermique de medicament Download PDFInfo
- Publication number
- CA3112808A1 CA3112808A1 CA3112808A CA3112808A CA3112808A1 CA 3112808 A1 CA3112808 A1 CA 3112808A1 CA 3112808 A CA3112808 A CA 3112808A CA 3112808 A CA3112808 A CA 3112808A CA 3112808 A1 CA3112808 A1 CA 3112808A1
- Authority
- CA
- Canada
- Prior art keywords
- formulation
- basement membrane
- active ingredient
- agent
- penetration
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 238000013271 transdermal drug delivery Methods 0.000 title description 5
- 239000003795 chemical substances by application Substances 0.000 claims abstract description 108
- 239000000203 mixture Substances 0.000 claims abstract description 107
- 210000002469 basement membrane Anatomy 0.000 claims abstract description 104
- 238000009472 formulation Methods 0.000 claims abstract description 90
- 239000004480 active ingredient Substances 0.000 claims abstract description 86
- 230000035515 penetration Effects 0.000 claims abstract description 68
- 210000003491 skin Anatomy 0.000 claims abstract description 60
- 210000004207 dermis Anatomy 0.000 claims abstract description 46
- 238000000034 method Methods 0.000 claims abstract description 36
- 230000037317 transdermal delivery Effects 0.000 claims abstract description 36
- 210000001519 tissue Anatomy 0.000 claims abstract description 34
- 210000002615 epidermis Anatomy 0.000 claims abstract description 24
- 210000000434 stratum corneum Anatomy 0.000 claims abstract description 22
- 239000002904 solvent Substances 0.000 claims abstract description 19
- 239000012528 membrane Substances 0.000 claims abstract description 4
- 210000004379 membrane Anatomy 0.000 claims abstract description 3
- 230000004888 barrier function Effects 0.000 claims description 32
- -1 propentofyltine Chemical compound 0.000 claims description 23
- 239000003071 vasodilator agent Substances 0.000 claims description 22
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims description 21
- 229940124549 vasodilator Drugs 0.000 claims description 21
- RPTUSVTUFVMDQK-UHFFFAOYSA-N Hidralazin Chemical compound C1=CC=C2C(NN)=NN=CC2=C1 RPTUSVTUFVMDQK-UHFFFAOYSA-N 0.000 claims description 18
- 239000005526 vasoconstrictor agent Substances 0.000 claims description 17
- 241000124008 Mammalia Species 0.000 claims description 16
- XQYZDYMELSJDRZ-UHFFFAOYSA-N papaverine Chemical compound C1=C(OC)C(OC)=CC=C1CC1=NC=CC2=CC(OC)=C(OC)C=C12 XQYZDYMELSJDRZ-UHFFFAOYSA-N 0.000 claims description 14
- 239000000126 substance Substances 0.000 claims description 14
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- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 13
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- VYFYYTLLBUKUHU-UHFFFAOYSA-N dopamine Chemical compound NCCC1=CC=C(O)C(O)=C1 VYFYYTLLBUKUHU-UHFFFAOYSA-N 0.000 claims description 12
- BNRNXUUZRGQAQC-UHFFFAOYSA-N sildenafil Chemical compound CCCC1=NN(C)C(C(N2)=O)=C1N=C2C(C(=CC=1)OCC)=CC=1S(=O)(=O)N1CCN(C)CC1 BNRNXUUZRGQAQC-UHFFFAOYSA-N 0.000 claims description 12
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- VZGDMQKNWNREIO-UHFFFAOYSA-N tetrachloromethane Chemical compound ClC(Cl)(Cl)Cl VZGDMQKNWNREIO-UHFFFAOYSA-N 0.000 claims description 8
- 229930008281 A03AD01 - Papaverine Natural products 0.000 claims description 7
- XEYBHCRIKKKOSS-UHFFFAOYSA-N disodium;azanylidyneoxidanium;iron(2+);pentacyanide Chemical compound [Na+].[Na+].[Fe+2].N#[C-].N#[C-].N#[C-].N#[C-].N#[C-].[O+]#N XEYBHCRIKKKOSS-UHFFFAOYSA-N 0.000 claims description 7
- OSWPMRLSEDHDFF-UHFFFAOYSA-N methyl salicylate Chemical compound COC(=O)C1=CC=CC=C1O OSWPMRLSEDHDFF-UHFFFAOYSA-N 0.000 claims description 7
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- 239000003880 polar aprotic solvent Substances 0.000 claims description 7
- 229940083618 sodium nitroprusside Drugs 0.000 claims description 7
- XMGQYMWWDOXHJM-JTQLQIEISA-N (+)-α-limonene Chemical compound CC(=C)[C@@H]1CCC(C)=CC1 XMGQYMWWDOXHJM-JTQLQIEISA-N 0.000 claims description 6
- KWGRBVOPPLSCSI-WPRPVWTQSA-N (-)-ephedrine Chemical compound CN[C@@H](C)[C@H](O)C1=CC=CC=C1 KWGRBVOPPLSCSI-WPRPVWTQSA-N 0.000 claims description 6
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- CNIIGCLFLJGOGP-UHFFFAOYSA-N 2-(1-naphthalenylmethyl)-4,5-dihydro-1H-imidazole Chemical compound C=1C=CC2=CC=CC=C2C=1CC1=NCCN1 CNIIGCLFLJGOGP-UHFFFAOYSA-N 0.000 claims description 6
- GIKNHHRFLCDOEU-UHFFFAOYSA-N 4-(2-aminopropyl)phenol Chemical compound CC(N)CC1=CC=C(O)C=C1 GIKNHHRFLCDOEU-UHFFFAOYSA-N 0.000 claims description 6
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- 239000004475 Arginine Substances 0.000 claims description 6
- JZUFKLXOESDKRF-UHFFFAOYSA-N Chlorothiazide Chemical compound C1=C(Cl)C(S(=O)(=O)N)=CC2=C1NCNS2(=O)=O JZUFKLXOESDKRF-UHFFFAOYSA-N 0.000 claims description 6
- AOJJSUZBOXZQNB-TZSSRYMLSA-N Doxorubicin Chemical compound O([C@H]1C[C@@](O)(CC=2C(O)=C3C(=O)C=4C=CC=C(C=4C(=O)C3=C(O)C=21)OC)C(=O)CO)[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 AOJJSUZBOXZQNB-TZSSRYMLSA-N 0.000 claims description 6
- XBLVHTDFJBKJLG-UHFFFAOYSA-N Ethyl nicotinate Chemical compound CCOC(=O)C1=CC=CN=C1 XBLVHTDFJBKJLG-UHFFFAOYSA-N 0.000 claims description 6
- UGJMXCAKCUNAIE-UHFFFAOYSA-N Gabapentin Chemical compound OC(=O)CC1(CN)CCCCC1 UGJMXCAKCUNAIE-UHFFFAOYSA-N 0.000 claims description 6
- ODKSFYDXXFIFQN-BYPYZUCNSA-P L-argininium(2+) Chemical compound NC(=[NH2+])NCCC[C@H]([NH3+])C(O)=O ODKSFYDXXFIFQN-BYPYZUCNSA-P 0.000 claims description 6
- ZFMITUMMTDLWHR-UHFFFAOYSA-N Minoxidil Chemical compound NC1=[N+]([O-])C(N)=CC(N2CCCCC2)=N1 ZFMITUMMTDLWHR-UHFFFAOYSA-N 0.000 claims description 6
- LRHPLDYGYMQRHN-UHFFFAOYSA-N N-Butanol Chemical compound CCCCO LRHPLDYGYMQRHN-UHFFFAOYSA-N 0.000 claims description 6
- CHJJGSNFBQVOTG-UHFFFAOYSA-N N-methyl-guanidine Natural products CNC(N)=N CHJJGSNFBQVOTG-UHFFFAOYSA-N 0.000 claims description 6
- MWUXSHHQAYIFBG-UHFFFAOYSA-N Nitric oxide Chemical compound O=[N] MWUXSHHQAYIFBG-UHFFFAOYSA-N 0.000 claims description 6
- 229940025084 amphetamine Drugs 0.000 claims description 6
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- KVYGGMBOZFWZBQ-UHFFFAOYSA-N benzyl nicotinate Chemical compound C=1C=CN=CC=1C(=O)OCC1=CC=CC=C1 KVYGGMBOZFWZBQ-UHFFFAOYSA-N 0.000 claims description 6
- AYMYWHCQALZEGT-ORCRQEGFSA-N butein Chemical compound OC1=CC(O)=CC=C1C(=O)\C=C\C1=CC=C(O)C(O)=C1 AYMYWHCQALZEGT-ORCRQEGFSA-N 0.000 claims description 6
- 230000003196 chaotropic effect Effects 0.000 claims description 6
- ZPUCINDJVBIVPJ-LJISPDSOSA-N cocaine Chemical compound O([C@H]1C[C@@H]2CC[C@@H](N2C)[C@H]1C(=O)OC)C(=O)C1=CC=CC=C1 ZPUCINDJVBIVPJ-LJISPDSOSA-N 0.000 claims description 6
- KWGRBVOPPLSCSI-UHFFFAOYSA-N d-ephedrine Natural products CNC(C)C(O)C1=CC=CC=C1 KWGRBVOPPLSCSI-UHFFFAOYSA-N 0.000 claims description 6
- 229960004042 diazoxide Drugs 0.000 claims description 6
- SWSQBOPZIKWTGO-UHFFFAOYSA-N dimethylaminoamidine Natural products CN(C)C(N)=N SWSQBOPZIKWTGO-UHFFFAOYSA-N 0.000 claims description 6
- 229960003638 dopamine Drugs 0.000 claims description 6
- 229960004198 guanidine Drugs 0.000 claims description 6
- 150000002357 guanidines Chemical class 0.000 claims description 6
- CGIGDMFJXJATDK-UHFFFAOYSA-N indomethacin Chemical compound CC1=C(CC(O)=O)C2=CC(OC)=CC=C2N1C(=O)C1=CC=C(Cl)C=C1 CGIGDMFJXJATDK-UHFFFAOYSA-N 0.000 claims description 6
- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 claims description 6
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- YNBADRVTZLEFNH-UHFFFAOYSA-N methyl nicotinate Chemical compound COC(=O)C1=CC=CN=C1 YNBADRVTZLEFNH-UHFFFAOYSA-N 0.000 claims description 6
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- WYWIFABBXFUGLM-UHFFFAOYSA-N oxymetazoline Chemical compound CC1=CC(C(C)(C)C)=C(O)C(C)=C1CC1=NCCN1 WYWIFABBXFUGLM-UHFFFAOYSA-N 0.000 claims description 6
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Classifications
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- A61K9/70—Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
- A61K9/7023—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms
- A61K9/703—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms characterised by shape or structure; Details concerning release liner or backing; Refillable patches; User-activated patches
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- A61K31/155—Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
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- A61K31/19—Carboxylic acids, e.g. valproic acid
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- A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
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- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
- A61K31/52—Purines, e.g. adenine
- A61K31/522—Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
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- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
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- A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
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- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
- A61K47/18—Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
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Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
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- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
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- Engineering & Computer Science (AREA)
- Dermatology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- General Chemical & Material Sciences (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Emergency Medicine (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
La présente invention concerne des systèmes, des méthodes et des kits d'administration transdermique qui comprennent un agent qui permet de pénétrer dans la membrane basale, une membrane de la peau auparavant décrite comme difficile à pénétrer. En particulier, la formulation comprend un perturbateur de la membrane basale qui dénature de manière réversible la membrane basale de la peau. La formulation de la présente invention comprend en outre au moins un agent de pénétration, au moins un vaso-modulateur et au moins un principe actif. Dans un mode de réalisation, l'agent de pénétration comprend un solvant, un agent lipophile, un agent hydrophile, le perturbateur de la membrane basale, le modulateur vasculaire et le principe actif passant à travers la couche cornée et l'épiderme. Le perturbateur de la membrane basale permet au modulateur vasculaire et au principe actif de passer à travers la membrane basale afin de pénétrer dans le derme. Le principe actif, une fois au niveau du derme, est administré localement au tissu ou de façon systémique au flux sanguin.
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
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US201862737479P | 2018-09-27 | 2018-09-27 | |
US62/737,479 | 2018-09-27 | ||
US16/582,922 | 2019-09-25 | ||
PCT/US2019/053000 WO2020069013A1 (fr) | 2018-09-27 | 2019-09-25 | Système d'administration transdermique de médicament |
US16/582,922 US11446257B2 (en) | 2018-09-27 | 2019-09-25 | Transdermal drug delivery system |
Publications (1)
Publication Number | Publication Date |
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CA3112808A1 true CA3112808A1 (fr) | 2020-04-02 |
Family
ID=69947952
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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CA3112808A Pending CA3112808A1 (fr) | 2018-09-27 | 2019-09-25 | Systeme d'administration transdermique de medicament |
Country Status (5)
Country | Link |
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US (3) | US11446257B2 (fr) |
AU (1) | AU2019349935B2 (fr) |
CA (1) | CA3112808A1 (fr) |
MX (1) | MX2021002833A (fr) |
WO (1) | WO2020069013A1 (fr) |
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AU2019349935B2 (en) | 2018-09-27 | 2023-01-12 | BioPhysics Pharma, Inc. | Transdermal drug delivery system |
US11116737B1 (en) | 2020-04-10 | 2021-09-14 | University Of Georgia Research Foundation, Inc. | Methods of using probenecid for treatment of coronavirus infections |
CN112353767A (zh) * | 2020-11-16 | 2021-02-12 | 海南锦瑞制药有限公司 | 一种盐酸地尔硫卓和普瑞巴林组合物及其制备方法及其应用 |
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US3903159A (en) | 1970-09-17 | 1975-09-02 | Armour Pharma | Methanesulfonamidophenyl guanidine compounds |
US5460821A (en) | 1993-06-23 | 1995-10-24 | Masiz; John J. | Molecular transdermal transport system |
WO1995000088A1 (fr) | 1993-06-23 | 1995-01-05 | Masiz John J | Systeme de transport transdermique d'une molecule |
US5645854A (en) | 1993-06-23 | 1997-07-08 | Masiz; John J. | Molecular transdermal transport system |
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AU2019349935A1 (en) | 2021-03-18 |
US11865217B2 (en) | 2024-01-09 |
BR112021003746A2 (pt) | 2021-05-25 |
US20240108588A1 (en) | 2024-04-04 |
US20220387343A1 (en) | 2022-12-08 |
WO2020069013A1 (fr) | 2020-04-02 |
AU2019349935B2 (en) | 2023-01-12 |
US11446257B2 (en) | 2022-09-20 |
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